Ionic inhibitors of human leukocyte elastase: pyridinium and phenyl carboxylate derivatives of 3-alkyl-N-hydroxysuccinimide.
A series of pyridinium and phenyl carboxylate derivatives of 3-alkyl-N-hydroxysuccinimide has been synthesized; the compounds have been shown to be highly effective, time-dependent inactivators of human leukocyte elastase. The cationic inhibitor having an isobutyl side chain as the P1 residue (3) was found to be the most effective. Human leukocyte cathepsin G and chymotrypsin are also inactivated by these compounds.
Groutas
W C
WC
Department of Chemistry, Wichita State University, KS 67208.
Stanga
M A
MA
Castrisos
J C
JC
Schatz
E J
EJ
Brubaker
M J
MJ
D001565:Benzoates / Q000138:chemical synthesis / Q000494:pharmacology*; D056649:Cathepsin G; D002403:Cathepsins / Q000037:antagonists & inhibitors; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D002918:Chymotrypsin / Q000037:antagonists & inhibitors; D006801:Humans; D066298:In Vitro Techniques; D007962:Leukocytes / Q000201:enzymology*; D009682:Magnetic Resonance Spectroscopy; D010196:Pancreatic Elastase / Q000037:antagonists & inhibitors*; D011726:Pyridinium Compounds / Q000138:chemical synthesis / Q000494:pharmacology*; D012697:Serine Endopeptidases; D013388:Succinimides / Q000138:chemical synthesis / Q000494:pharmacology*
D001565:Benzoates; D011726:Pyridinium Compounds; D013388:Succinimides; D002403:Cathepsins; D012697:Serine Endopeptidases; D002918:Chymotrypsin; C534094:CTSG protein, human; D056649:Cathepsin G; D010196:Pancreatic Elastase